C07D241/08

METHOD FOR RACEMIC PREPARATION OF CHIRAL B-AMINO ACIDS AND DERIVATIVES THEREOF
20230142248 · 2023-05-11 ·

The present disclosure relates to the field of medicine synthesis, and relates to a method for a racemic preparation of chiral h β-amino acids and derivatives thereof, and in particular to a method for racemizing sitagliptin intermediates.

##STR00001##

where R.sub.1 is hydrogen, alkyl or aryl; R.sub.2 is hydrogen, alkyl or aryl; R.sub.3 is hydrogen, alkyl, aryl or acyl; R.sub.4 is alkyl, aryl, OR′, SR′, NHR′ or NR′R″, wherein R′, R″ are hydrogen, alkyl or aryl.

Alkenyl substituted 2,5-piperazinediones, compositions, and uses thereof

Provided herein are compounds of Formula (I), and salts thereof, wherein each instance of R.sup.L is independently optionally substituted C.sub.6-C.sub.40 alkenyl. Further provided are compositions comprising a compound of Formula (I) and an agent. Further provided are methods and kits using the compositions for delivering an agent to a subject or cell and for treating and/or preventing a range of diseases. Further provided are methods of preparing compounds of Formula (I) and precursors thereof. ##STR00001##

Alkenyl substituted 2,5-piperazinediones, compositions, and uses thereof

Provided herein are compounds of Formula (I), and salts thereof, wherein each instance of R.sup.L is independently optionally substituted C.sub.6-C.sub.40 alkenyl. Further provided are compositions comprising a compound of Formula (I) and an agent. Further provided are methods and kits using the compositions for delivering an agent to a subject or cell and for treating and/or preventing a range of diseases. Further provided are methods of preparing compounds of Formula (I) and precursors thereof. ##STR00001##

Polyamine-fatty acid derived lipidoids and uses thereof

The present disclosure provides polyamine-fatty acid derived lipidoids (e.g., compounds of Formula (I) or (II)) and methods of preparing the lipidoids. A described lipidoid includes R—C(═O)—O— moieties (where R is a lipid moiety), which may be hydrolyzed into non-toxic fatty acids. Also provided are compositions including a described lipidoid and an agent (e.g., polynucleotide, small molecule, peptide, or protein). The present disclosure also provides methods, kits, and uses that involve the lipidoids or compositions for delivering an agent to a subject, tissue, or cell and/or for treating and/or preventing a range of diseases, such as genetic diseases, proliferative diseases, hematological diseases, neurological diseases, immunological diseases, gastrointestinal diseases, respiratory diseases, painful conditions, psychiatric disorders, and metabolic disorders. ##STR00001##

Polyamine-fatty acid derived lipidoids and uses thereof

The present disclosure provides polyamine-fatty acid derived lipidoids (e.g., compounds of Formula (I) or (II)) and methods of preparing the lipidoids. A described lipidoid includes R—C(═O)—O— moieties (where R is a lipid moiety), which may be hydrolyzed into non-toxic fatty acids. Also provided are compositions including a described lipidoid and an agent (e.g., polynucleotide, small molecule, peptide, or protein). The present disclosure also provides methods, kits, and uses that involve the lipidoids or compositions for delivering an agent to a subject, tissue, or cell and/or for treating and/or preventing a range of diseases, such as genetic diseases, proliferative diseases, hematological diseases, neurological diseases, immunological diseases, gastrointestinal diseases, respiratory diseases, painful conditions, psychiatric disorders, and metabolic disorders. ##STR00001##

Diketopiperazine Microparticles with Defined Specific Surface Areas

Disclosed herein are diketopiperazine microparticles having a specific surface area of less than about 67 m.sup.2/g. The diketopiperazine microparticle can be fumaryl diketopiperazine and can comprise a drug such as insulin.

Diketopiperazine Microparticles with Defined Specific Surface Areas

Disclosed herein are diketopiperazine microparticles having a specific surface area of less than about 67 m.sup.2/g. The diketopiperazine microparticle can be fumaryl diketopiperazine and can comprise a drug such as insulin.

N-acyl amino acid compounds and methods of use

The invention relates to compounds of formula (I): ##STR00001##
or a salt thereof, wherein R.sup.1, A, L, and R.sup.2 and n are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are αvβ1 integrin inhibitors that are useful for treating tissue specific fibrosis.